Citrus fruit and fabacea secondary metabolites potently and selectively block TRPM3.

ABSTRACT:

Background and purpose

The melastatin-related transient receptor potential TRPM3 is a calcium-permeable nonselective cation channel that can be activated by the neurosteroid pregnenolone sulphate (PregS) and heat. TRPM3-deficient mice show an impaired perception of noxious heat. Hence, drugs inhibiting TRPM3 possibly get in focus of analgesic therapy.

Experimental approach

Fluorometric methods were used to identify novel TRPM3-blocking compounds and to characterize their potency and selectivity to block TRPM3 but not other sensory TRP channels. Biophysical properties of the block were assessed using electrophysiological methods. Single cell calcium measurements confirmed the block of endogenously expressed TRPM3 channels in rat and mouse dorsal root ganglion (DRG) neurones.<

SUBMITTER: Straub I 

PROVIDER: S-EPMC3623054 | biostudies-literature | 2013 Apr

REPOSITORIES: biostudies-literature